Antibacterial, Antifungal, and Antioxidant Activity of Cleome coluteoides: An In Vitro Comparative Study Between Leaves, Stems, and Flowers.

OBJECTIVES: Cleome coluteoides, which belongs to the Capparidaceae family, and has been used in folk medicine for a long time. Our research aims to measure the antioxidant, antibacterial, and antifungal activities of C. coluteoides. MATERIALS AND METHODS: Various solvents, such as ethyl acetate, methanol, and dichloromethane, were used to extract different plant parts. Antibacterial and antifungal activities were assayed by disk and well diffusion methods, and the antioxidant activity was screened by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing ability of plasma methods. RESULTS: Results showed that Gram-negative bacteria and fungus were resistant to various plant extracts. Against all Gram-positive bacteria tested, C. coluteoides' flower extract had the highest inhibition effects. Also, the most sensitive bacterium was Bacillus cereus, which had an 18-mm inhibition zone. Due to the solvent's physical and chemical properties, different C. coluteoides extracts exhibited various antioxidant activities in the antioxidant activity assay. To some extent, methanol extract of leaves showed the highest DPPH radical scavenging activity at various concentrations that ranged from 5 to 160 mg.mL-1. The methanol extract of flower was observed to have the highest level of phenolics among all tested extracts. CONCLUSION: This study demonstrates that different extracts from various C. coluteoides parts are different in their properties, therefore, a proper solvent should be used to extract maximum amounts of antioxidant and antibacterial components from a typical plant material.

Role of Herbal Medicines in the Management of Brain Injury.

Brain is susceptible to oxidative stress due to its increased oxygen consumption and low antioxidant levels. Oxidative stress plays a crucial role in the pathogenesis of various neurological diseases. This review on the role of herbal medicines in the management of brain injury was performed by searching Web of Science, PubMed, Google Scholar, Scopus, and Iran Medex between 1976 to January 2020. The search words contained brain injury, and the total number of publications for the review study was 32. Studies with various medicinal plants such as Acanthopanax senticosus, Bacopa monnieri, carnosol, Cassia mimosoides, Centella asiatica, Crocus sativus, Cuminum cyminum, curcumin, Feronia limonia, Gardenia jasminoides, Ginkgo biloba, Kaempferia parviflora, Mentha longifolia, Nigella sativa, olive, orientin, pomegranate, quercetin, rice bran, Rosa damascena, Thymus vulgaris, Viola odorata, Withania coagulans, Zingiber officinale, and Ziziphus spina-christi show a significant improvement in brain injury. The different mechanisms for improvement in brain injury by these medicinal plants include HIF-1 (hypoxia-inducible factor 1) signaling, free-radical scavenging, reduction of nitric oxide (NO) toxicity and acetylcholine esterase (AChE) activity, decrease of pAkt and its downstream targets, downregulation of the aquaporin-4 (AQP-4) and TLR4/NF-ĸB/TNF-α signal, reduction in malondialdehyde and NO levels, increasing neuronal density in the hippocampus, and inhibition of oxidative stress. In this review, the neuroprotective actions and molecular mechanisms of herbal medicines are evaluated by reviewing available studies.

MLC901 during sleep deprivation rescues fear memory disruption in rats.

Several lines of evidence suggest that sleep deprivation disrupts cognitive and emotional abilities and changes the expression of distinctive categories of genes in the brain. In the present study, saline- or MLC901 (a traditional Chinese medicine)-treated male Wistar rats were first submitted to a modified water box (for 24-h sleep deprivation) and then trained in contextual and tone fear conditioning tasks with the purpose to evaluate the effect of MLC901 during sleep deprivation on fear memory retention. Hippocampal mRNA measurement was performed by reverse transcription-polymerase chain reaction (RT-PCR). We found that the exposure of rats to 24 h of sleep deprivation impaired contextual and tone fear memory retention, while administration of MLC901 (0.2, 0.4, and 0.8 mg/kg, once/12 h; i.p.) during sleep deprivation abolished memory deficits. Meanwhile, different doses of MLC901 alone had no effect on performance in both tasks. We observed that MLC901 increased the expression levels of pro-apoptotic BAD, anti-apoptotic Bcl-xL, and Tfam as an index of mitochondrial biogenesis compared to sleep-deprived rats, while MLC901 during sleep deprivation increased BAX, BAD, and Bcl-xL compared to the control group. Sleep deprivation decreased BAX and Tfam, by itself. MLC901 only decreased BAX and Tfam and increased BAD level compared to the non-sleep-deprived control group. It is suggested that MLC901 might be a therapeutic option for memory impairment during sleep deprivation.

Tongluojiunao, a traditional Chinese medication with neuroprotective ability: A review of the cellular, molecular and physiological mediators of TLJN's effectiveness.

The pressing need to discover more effective drugs for various CNS disorders has resurrected the idea of investigating the effectiveness of traditional medicines in modern science. Tongluojiunao (TLJN) is an example of revived modern herbal preparation based on traditional Chinese medicine (TCM) with a long history of administration for various types of cerebrovascular injuries and neurodegenerative diseases. TLJN is prepared from the herbal roots of Panax notoginseng (Sanchi) and dried fruits of Gardenia jasminoides (Cape Jasmine), and so far, it has demonstrated promising results in patients with vascular dementia and cerebral ischemic stroke. TLJN has also demonstrated therapeutic ability regarding the slowly-progressed neurodegenerative diseases like Alzheimer's disease. So it tempted us to undertake a thorough review of various features of TLJN therapeutic effects on the mentioned CNS conditions, including the cellular and molecular targets, inflammatory responses, neurogenesis and angiogenesis mediators and cognitive function. For this purpose, multiple global and local databases, including China National Knowledge Infrastructure (CNKI) were checked out and the retrieved information was grouped according to their scope of studies. Among these, TLJN is reported to restore the deregulated cell-cell communication in the neurovascular unit, prevent the stress-related challenges imposed by ischemia/reperfusion insult, help with the cerebral tissue recovery after traumatic brain damage, avoid the epileptic seizure attack and limit the progression of Alzheimer's disease. We hope that the current review provides new insights into TLJN medication as a prospective neuroprotective medication for further more in-depth investigation in the future.

Biological activities of farnesiferol C: a review.

Farnesiferol C (FC) is a sesquiterpene coumarin, with a unique chemical structure, isolated from Ferula (Apiaceae) species including Ferula assa-foetida and Ferula szowitsiana. The compound is an important natural product with different biological activities. Recently, researchers have been interested in FC and begun to investigate its biological effects. They have shown that FC possesses various biological properties including cytotoxic, apoptotic, MDR reversal, antitumor, antimutagenic, and antiviral activity. In addition, FC has shown moderate neuroprotective activity against oxygen-glucose deprivation in vitro. This review summarizes the biological activities of FC that has been published to date. A complete search performed on relevant databases consists of Pubmed, Scopus, Web of science, Google scholar, Science direct, and Magiran. Selected keywords were sesquiterpene coumarin, farnesiferol C, biological activity, cytotoxicity, pharmacology, anticancer, and anti-angiogenesis. All of the data were checked out and irrelevant articles were discarded.

In vitro antioxidant and antibacterial activity of various extracts from exocarps and endocarps of walnut.

Juglans regia seed has been used in traditional medicines as antimicrobial, antihelmintic and anti-diarrhoeal. In the present study, the antibacterial capabilities dichloromethane, ethyl acetate, methanol and aqueous extracts of endocarp and exocarp of walnut were determined against two Gram-positive bacteria and one Gram-negative bacteria. The antioxidant activity was screened by 2, 2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and ferric reducing antioxidant power (FRAP) assays. The highest antioxidant activity was observed for methanol extract of endocarp in both methods and it was stronger than positive control butylated hydroxy toluene (BHT). The total phenolic contents were ranging between 34.59 to 68.34mg GAE/g DW. The results revealed that all extracts had antibacterial activity against selected bacteria except aqueous extract. The methanol extract of endocarp presented the highest zone of inhibition against tested pathogens (9-21mm). From the results it is conclude that the methanol extract from endocarp of walnut could be used as a natural preservative ingredient in food and pharmaceutical industries.

Phytochemical screening and evaluation of antioxidant activities of Dracocephalum kotschyi and determination of its luteolin content.

OBJECTIVE: Dracocephalum kotschyi (Lamiaceae family) has been used in traditional medicine for stomach and liver disorders, headache and congestion. In the present study, we have investigated phytochemical properties and antioxidant activities of dichloromethane, ethyl acetate and methanol extracts of D.kotschyi. MATERIAL AND METHODS: Antioxidant activities of extracts were evaluated using the integration of HPLC-DPPH and ferric reducing antioxidant power (FRAP) methods. In addition, the luteolincontent was determined using HPLC method. RESULTS: The highest antioxidant activity was observed for the methanol extract (among the three tested extracts) showing 50% DPPH scavenging activity at 4.85µg/ml as compared to butylated hydroxy toluene (BHT) and ascorbic acid (3.00 µg/ml, 0.97 µg/ml). Also, luteolin was detected in methanol extract; it was identified by comparing its retention time and DAD spectra with standard and it was one of antioxidant components of this plant. In addition, the antioxidant activity of methanol extract was higher than BHT, in FRAP assay. Total phenolic content was in the range of 11.62-22.29 mg Gallic acid /gram of dry extract and flavonoid content was in the range of 3.97-5.042 mg Quercetin/ gram of extract for dichloromethane, ethyl acetate and methanol extracts. The quantity of luteolin in D.kotschyiwas found to be 1061.005 µg/g of dried plant. CONCLUSION: The results of this investigation indicated that luteolin plays major role in the antioxidant activity of the plant.

Evaluation of the cytotoxic effects of Cyperus longus extract, fractions and its essential oil on the PC3 and MCF7 cancer cell lines.

Cyperus longus is one of the Iranian endemic species. However, to date, and to the best of our knowledge, there are no availale academic reports on the cytotoxicity of this plant. Thus, this study was carried out to examine the in vitro anti-proliferative and anti-apoptotic effects of Cyperus longus extract, fractions and essential oil (EO) on MCF7 and PC3 cell lines. The chemical constituents of EO were identified using gas chromatography (GC)-mass spectrometry (MS) analysis. The cells were cultured in RPMI-1640 medium and incubated with various concentrations of the plant extract and fractions. Cell viability was quantified by MTT assay following 24, 48 and 72 h of exposure to (12.5-200 µg/ml) of the methanol extract, the dichloromethane (CH2Cl2), ethyl acetate (EtOAc) and water fractions, as well as the EO of the plant. The percentage of apoptotic cells was determined using propidium iodide staining of DNA fragments by flow cytometry (sub-G1 peak). The most effective fraction in the MCF7 cell line was the CH2Cl2 fraction (IC50 after 48 h, 25.34±2.01). The EtOAc fraction (IC50 after 48 h, 35.2±2.69) and the methanol extract (IC50 after 48 h, 64.64±1.64) were also found to be effective. The IC50 values obtained for the PC3 cell line were 37.97±3.87, 51.57±3.87 and 70.33±2.36 for the CH2Cl2 fraction, the EtOAc fraction and the methanol extract, respectively. Based on these data and due to the partial polarity of the most effective fraction (the CH2Cl2 fraction), we also examined the cytotoxicity of the plant EO. The IC50 values after 48 h were 22.25±4.25 and 12.55±3.65 in the PC3 and MCF7 cell lines, respectively. DNA fragmentation assay also confirmed these data. Performing GC-MS analysis for the plant EO revealed that ß-himachalene (10.81%), α-caryophyllene oxide (7.6%), irisone (4.78%), ß-caryophyllene oxide (4.36%), humulene oxide (12%), viridiflorol (4.73%), aristolone (6.39%) and longiverbenone (6.04%) were the main constituents. Our results demonstrated that two of the constituents of Cyperus longus, viridiflorol and longiverbenone, should be investigated further as possible promising chemotherapeutic agents in cancer treatment.

Effects of hydro-alcoholic extract of Launaea acanthodes on serum gonadotropin and testosterone levels and the structure of seminiferous tubules in hyperglycemic rats.

OBJECTIVE: To investigate the effects of hydro-alcoholic extract of Launaea acanthodes, a blood glucose lowering plant in folk medicine of Iran, on the structure of seminiferous tubules and serum gonadotropin and testosterone levels in hyperglycemic rats. METHODS: Twenty-four Wistar rats were randomly allocated into 4 groups (n=6): control, streptozotocin (STZ), STZ + insulin [STZ + Ins, 5 IU/(kg•day)], and STZ + Launaea acanthodes extract [STZ + Ext, 150 mg/(kg•day)]. Blood samples were collected at the 2nd and 4th weeks for detection of testosterone, follicle stimulating hormone (FSH) and luteinizing hormone (LH) with enzyme-linked immuno sorbent assay (ELISA), and the right testes of rats were removed at the 7th week for the evaluation of diameter and wall thickness of seminiferous tubules and number of Leydig cells using unbiased stereological techniques. RESULTS: In comparison with the control group, at the 2nd week FSH (0.45 vs 0.03, 0.02, 0.02 IU/L in STZ, STZ + Ins and STZ + Ext groups, respectively) and LH (1.02 vs 0.37, 0.2, 0.29 IU/L) showed significant decreases (all P<0.05) and testosterone (4.2 vs 8.37, 7.78, 11.8 ng/mL) showed a remarkable increase (all P<0.05). The levels of these hormones became closer in the STZ + Ext and the STZ + Ins groups to the control at the 4th week. A significant decrease in diameter and wall thickness of seminiferous tubules and number of Leydig cells were observed in the STZ group as compared with the control (P<0.01). CONCLUSIONS: Administration of Launaea extract demonstrated a beneficial impact on the protection of testis from pathogenic and degenerative effects of hyperglycemia which may be partly due to its potential antioxidative effects.

Growth inhibition and apoptosis induction by Scutellaria pinnatifida A. Ham. on HL-60 and K562 leukemic cell lines.

A rich flavonoid plant extensively used in traditional medicine is Scutellaria (Lamiaceae). In this study the cytotoxic effects of different extracts of Scutellaria pinnatifida were explored on two different cancer cell lines including K562 and HL-60 and a normal cell line. Also, the role of apoptosis on this toxicity was explored. The cell viability was quantitated by alamarBlue(®) assay. S. pinnatifida could effectively decrease the viability of malignant cells and the CH2Cl2 extract of S. pinnatifida had showed the most cytotoxic effects among other extracts. Apoptosis was confirmed after propidium iodide staining of DNA fragments and detection of the sub-G1 peak in the related flow cytometry histogram of cells. The results of western blot assay showed that CH2Cl2 extract has been able to increase the amount of Bax and cleavage of PARP protein after a 48h contact with cells. Neobaicalein (skullcapflavone II) and wogonin were identified in the extract of S. pinnatifida as the active components. The result of the present study confirmed the putative role of neobaicalein (skullcapflavone II) and wogonin as cytotoxic components in the CH2Cl2 extract of S. pinnatifida.

Improvement of physicomechanical properties of carbamazepine by recrystallization at different pH values.

The morphology of crystals has an appreciable impact role on the physicochemical properties of drugs. Drug properties such as flowability, dissolution, hardness and bioavailability may be affected by crystallinity behaviours of drugs. The objective of this study was to achieve an improved physicomechanical property of carbamazepine powder through recrystallization from aqueous solutions at different pH values. For this purpose, carbamazapine was recrystallized from aqueous solutions at different pH values (1, 7, 11). The morphology of crystals was investigated using scanning electron microscopy; X-ray powder diffraction (XRPD) was used to identify polymorphism; thermodynamic properties were analyzed using differential scanning calorimetery (DSC). Dissolution rate was determined using USP dissolution apparatus. Mechanical behavior of recrystallized carbamazepine powders was investigated by making tablets under different compaction pressure and measuring their hardness. SEM studies showed that the carbamazepine crystallization in different media affected the morphology and size of carbamazepine crystals. The shape of carbamazepine crystals changed from flaky or thin plate-like to needle shape. XRPD and DSC results ruled out any crystallinity changes occurring due to the temperature during recrystallization procedure or pH of crystallization media. The crushing strength of tablets indicated that all of the recrystallized carbamazepine samples had better compactiblity than the original carbamazepine powder. In vitro dissolution studies of carbamazepine samples showed a higher dissolution rate for carbamazepine crystals obtained from media with pH 11 and 1. Carbamazepine particles recrystallized from aqueous solutions of different pH values (all media) appeared to have superior mechanical properties to those of the original carbamazepine sample.